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消旋15-甲基-17-苯基-18,19,20-失三碳前列腺素F2a甲酯及其15-差向异构体的合成

Synthesis of d,1-15-methyl-17-Phenyl-18,19,20-trinorProstagland in F2α methyl ester and Its 15-EPimer

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【作者】 吴元鎏; 杨光中; 金碧燕; 胡家玉; 王志蓉;

【Author】 Wu Yuanliu, Uang Guangzhong, Jin Biyan, Hu Chiayu andWang Zhirong(Institute of Materia Medica, Beijing)

【机构】 药物研究所; 药物研究所 北京; 北京; 北京;

【摘要】 <正> 我们曾报告了消旋17-苯-18,19,20-失三碳PGF2a甲酯(lA)及其15-差向异构体(1B)的合成[1]、[1A)对小鼠抗生育活性已大大超过其母体化合物PGF2α,与15-甲基PGF2a甲酯(IC)不相上下[2]。[1A]与(1A)与(1C)不

【Abstract】 Synthesis of d, 1-15-methy1-17-phenyl-18,19,20-trinorprostaglandin F2α methyl ester (6A) and its 15-epimer (6B) was reported.A mixture of (6A) and (6B) was obtained via a 4-step process,starting from α,β-unsaturated ketone( 2 ), with a total yield of 29%. The mixture was separated and purified with column chromatography on silica gel, to give(6A) and (6B) . Contrary to the usual manner, the Rf values of (3A) and (3B) on silica gel TLC were in the reversed order. Preliminary bioassay showed that (6A) and (6B) exhibited antifertility effect for terminating first trimester pregnancy in mice with a fertility rate of 10 and 60% respectively at a dose of 15/μ g/mouse S.C at days 6,7 and 8 of pregnany.

  • 【文献出处】 中国医学科学院学报 ,Acta Academiae Medicinae Sinicae , 编辑部邮箱 ,1985年02期
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